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Figure S1. (A) Detailed process for fitting the inhibition by QZ59-RRR of Hoechst 33342 efflux. (B) Fitting of the inhibition by QZ59-RRR of daunorubicin efflux.

Figure S2. (A) Fitting of the inhibition by QZ59-SSS of Hoechst 33342 efflux. (B) Fitting of the inhibition by QZ59-SSS of daunorubicin efflux.

Figure S3. (A) Hoechst 33342 docking on the mouse P-gp. (B) Daunorubicin docking on the mouse P-gp. (C) MTS rhodamine docking on the mouse P-gp.

Figure S4. Intracellular drugs quantitations.

Figure S5. Intracellular drug-substrate saturation.

Figure S6 (A) QZ59-SSS docking on the mouse P-gp. (B) QZ59-RRR docking on the mouse P-gp.

Table S1. Detailed results of the regression analyses.

Movie S1. Conformational changes of the mouse P-gp visualized by morphing.

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